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Cytochrome P-450 3A enzymes are responsible for biotransformation of FK506 and rapamycin in man and rat.
Abstract
The hepatic cytochrome P-450 responsible for metabolism of the structurally related macrolides FK506 and rapamycin in humans was identified using in vitro studies. FK506 and rapamycin metabolism was significantly correlated with nifedipine oxidation in human liver microsomes of eight different individuals. Immunoinhibition with anti-P450 3A4 abolished almost all FK506 and rapamycin metabolite formation. Inactivation of P450 3A4 by incubation of human liver microsomes with triacetyl oleandomycin (50 microM) or gestodene (10 microM) inhibited metabolism of FK506 and rapamycin. In liver microsomes from dexamethasone-treated rats FK506 and rapamycin metabolism was increased compared to liver microsomes from uninduced, phenobarbital-, or 3-methylcholanthrene-induced rats. FK506 and rapamycin were metabolized by reconstituted recombinant human liver P450 3A4. It is concluded that in human and rat liver FK506 and rapamycin are metabolized primarily by cytochrome P-450 3A4.
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Citations
Cited by
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Metadata
- Authors
- Sattler, M., Guengerich, F. P., Yun, C. H., Christians, U., & Sewing, K. F.
- Venue
- Drug Metabolism and Disposition
- Publisher
- Elsevier BV
- Published
- 1992-09
- Volume
- 20
- Issue
- 5
- Pages
- 753-761
- ISSN
- 0090-9556 (ISSN-L)
- OpenAlex
- W1872591512
- Cited by
- 385
- References
- 0
- FWCI
- 9.96
- Type
- journal article
- Language
- en
- Open access
- closed
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- CoChat. (2026). Citation check: Cytochrome P-450 3A enzymes are responsible for biotransformation of FK506 and rapamycin in man and rat. https://app.cochat.ai/papers/10.1016/s0090-9556(25)08793-8
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- Sattler, M., Guengerich, F. P., Yun, C. H., Christians, U., & Sewing, K. F. (1992). Cytochrome P-450 3A enzymes are responsible for biotransformation of FK506 and rapamycin in man and rat. Drug Metabolism and Disposition. https://doi.org/10.1016/s0090-9556(25)08793-8
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
